Propylene Glycol Liposomes as a Topical Delivery System for Miconazole Nitrate: Comparison with Conventional Liposomes
Propylene Glycol Liposomes as a Topical Delivery System for Miconazole Nitrate: Comparison with Conventional Liposomes
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DOI：
10.1208/s12249-012-9783-6
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发表时间：
2012-06-01
影响因子：
3.3
通讯作者：
Khalafallah, Nawal M.
中科院分区：
文献类型：
--
作者：
Elmoslemany, Riham M.;Abdallah, Ossama Y.;Khalafallah, Nawal M.
丙二醇（PG）-磷脂囊泡已被提倡作为柔性脂质囊泡用于增强药物的皮肤递送。为了进一步表征这些囊泡的性能并解决一些相关的药学问题，制备了硝酸咪康唑（MN）负载的PG纳米脂质体，并表征了囊泡大小、包封率、体外释放和囊泡稳定性。药物重要性的问题是丙二醇从囊泡中扩散出来的时间依赖性、稀释驱动性。这通过使用气相色谱法在分离的囊泡中评估丙二醇并在分离的囊泡在新鲜培养基中重复分散后监测其在培养基中的积聚来解决。此外，使用白色念珠菌评估所研究的脂质体制剂的抗真菌活性，并使用人皮肤研究其体外皮肤渗透和保留。在所有情况下，包括空白和载药常规脂质体用于比较。结果提供了受控的MN递送、在PG浓度范围2.5至10%的囊泡中恒定百分比的PG摄取（千分之45.5%）、改善的囊泡稳定性和以最小的皮肤渗透增强的MN的皮肤沉积的证据。这些是丙二醇-磷脂囊泡的不同配方和性能方面的关键问题。
Propylene glycol (PG)-phospholipid vesicles have been advocated as flexible lipid vesicles for enhanced skin delivery of drugs. To further characterize the performance of these vesicles and to address some relevant pharmaceutical issues, miconazole nitrate(MN)-loaded PG nanoliposomes were prepared and characterized for vesicle size, entrapment efficiency, in vitro release, and vesicle stability. An issue of pharmaceutical importance is the time-dependent, dilution-driven diffusion of propylene glycol out of the vesicles. This was addressed by assessing propylene glycol using gas chromatography in the separated vesicles and monitoring its buildup in the medium after repeated dispersion of separated vesicles in fresh medium. Further, the antifungal activity of liposomal formulations under study was assessed using Candida albicans, and their in vitro skin permeation and retention were studied using human skin. At all instances, blank and drug-loaded conventional liposomes were included for comparison. The results provided evidence of controlled MN delivery, constant percent PG uptake in the vesicles (a parts per thousand 45.5%) in the PG concentration range 2.5 to 10%, improved vesicle stability, and enhanced skin deposition of MN with minimum skin permeation. These are key issues for different formulation and performance aspects of propylene glycol-phospholipid vesicles.